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WAY-200070

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
WAY-200070
Clinical data
ATC code
  • None
Identifiers
  • 4-(7-Bromo-5-hydroxy-3H-1,3-benzoxazol-2-ylidene)cyclohexa-2,5-dien-1-one
CAS Number
PubChemCID
ChemSpider
UNII
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC13H8BrNO3
Molar mass306.115 g·mol−1
3D model (JSmol)
  • C1=CC(=CC=C1C2=NC3=CC(=CC(=C3O2)Br)O)O
  • InChI=1S/C13H8BrNO3/c14-10-5-9(17)6-11-12(10)18-13(15-11)7-1-3-8(16)4-2-7/h1-6,16-17H
  • Key:BAAILVWEAXFTSF-UHFFFAOYSA-N

WAY-200070 is asynthetic,nonsteroidal, highlyselectiveagonist ofERβ.[1][2] It possesses 68-fold selectivity for ERβ overERα (EC50 = 2 nM and 155 nM, respectively).[1] WAY-200070 has been found to enhanceserotonergic anddopaminergicneurotransmission in thecentral nervous system, and producesantidepressant- andanxiolytic-like effects in animals.[2] It has been proposed as a potential novel antidepressant/anxiolytic agent.[2] WAY-200070 has also been found to produceantidiabetic effects in animals,[3] and may also be beneficial for the treatment of certaininflammatory conditions.[1]

Due to its selectivity for ERβ, WAY-200070 is inactive in various assays of classicestrogen action, such asuterotrophic andosteopenia.[1] Moreover, WAY-200070 does not affectluteinizing hormone orfollicle-stimulating hormone or inhibitovulation, indicating that it does not suppress thehypothalamic-pituitary-gonadal axis, and as ERα and not ERβ is implicated inbreast development, would not be expected to cause growth of the breasts at doses that are selective for activation of ERβ.[4] In fact, ERβ activation may actually suppress breast growth,[4] and in accordance with this, WAY-200070 was shown to augment the efficacy oftamoxifen inin vitro models ofbreast cancer.[5] As such, WAY-200070 and other selective ERβ agonists might prove to be safe and tolerable for medical use in bothpremenopausal andpostmenopausal women and in individuals of either sex.

See also

[edit]

References

[edit]
  1. ^abcdMalamas MS, Manas ES, McDevitt RE, Gunawan I, Xu ZB, Collini MD, Miller CP, Dinh T, Henderson RA, Keith JC, Harris HA (2004). "Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-beta ligands".J. Med. Chem.47 (21):5021–40.doi:10.1021/jm049719y.PMID 15456246.
  2. ^abcHughes ZA, Liu F, Platt BJ,Dwyer JM, Pulicicchio CM, Zhang G, Schechter LE, Rosenzweig-Lipson S, Day M (2008). "WAY-200070, a selective agonist of estrogen receptor beta as a potential novel anxiolytic/antidepressant agent".Neuropharmacology.54 (7):1136–42.doi:10.1016/j.neuropharm.2008.03.004.PMID 18423777.S2CID 30469397.
  3. ^Alonso-Magdalena P, Ropero AB, García-Arévalo M, Soriano S, Quesada I, Muhammed SJ, Salehi A, Gustafsson JA, Nadal A (2013)."Antidiabetic actions of an estrogen receptor β selective agonist"(PDF).Diabetes.62 (6):2015–25.doi:10.2337/db12-1562.PMC 3661616.PMID 23349481.
  4. ^abHarris, Heather A. (2007)."Estrogen Receptor-β: Recent Lessons fromin Vivo Studies".Molecular Endocrinology.21 (1):1–13.doi:10.1210/me.2005-0459.ISSN 0888-8809.PMID 16556737.
  5. ^Lattrich C, Schüler S, Häring J, Skrzypczak M, Ortmann O, Treeck O (2014). "Effects of a combined treatment with tamoxifen and estrogen receptor β agonists on human breast cancer cell lines".Arch. Gynecol. Obstet.289 (1):163–71.doi:10.1007/s00404-013-2977-7.PMID 23907354.S2CID 35636541.


ERTooltip Estrogen receptor
Agonists
Mixed
(SERMsTooltip Selective estrogen receptor modulators)
Antagonists
GPERTooltip G protein-coupled estrogen receptor
Agonists
Antagonists
Unknown
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